| Cas No.: | 864864-17-5 |
| Chemical Name: | CFMTI |
| Synonyms: | 1H-Isoindol-1-one,2-cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-;CFMTI |
| SMILES: | O=C1N(C2CC2)CC3=C1C=CC(C4=C(C)N(C5=CC=CN=C5F)N=N4)=C3 |
| Formula: | C19H16FN5O |
| M.Wt: | 349.361646652222 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM. The selectivity of CFMTI to mGluR1 over mGluR5 was >2000-fold. |
| In Vivo: | CFMTI can dissolve in ethanol, polyethylene glycol 400, and distilled water (1:4:5, v/v/v) for intravenous administration. Oral administration of CFMTI inhibited DHPG-induced face-washing behavior in a dose-dependent manner. CFMTI produced dose-dependent inhibition of specific ex vivo binding of [3H]FTIDC to striatal and cerebellar slices in mice. CFMTI significantly inhibit hyperlocomotion induced by MAP at a dose of 2 mg/kg. |
| In Vitro: | The IC50 values of CFMTI against human mGluR5 were 5400 ± 1200 nM, showing that the activity of CFMTI is more than 2000-fold weaker against human mGluR5 than against human mGluR1. CFMTI up to 10 μM exhibited no agonistic activity toward any group I mGluR subtypes (data not shown). The IC50 values of CFMTI were higher than 10 μM against all targets, such as NMDA receptors |

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